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bioRxiv · 10.1101/2025.01.11.632537

An online GPCR drug discovery resource

Caroli, J.·Andreassen, S. N.·Lorente, J. S.·Xiao, B.·Pandy-Szekeres, G.·Gloriam, D.
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Abstract

G protein-coupled receptors (GPCRs) have been targeted across all therapeutic areas, mediate the actions of 516 (36% of all) approved drugs and are being targeted by 337 agents in clinical trials. So far, 121 GPCRs are targets of approved drugs and 30 additional receptors have entered clinical trials and may expand the drugged GPCRome in the coming years. Here, we describe an online resource of GPCR drugs, clinical trial agents, targets and disease indications. This resource offers unique reference data, analysis and visualization, and is availed as a new section, Drugs and Agents in trial integrated in the GPCR database, GPCRdb. Furthermore, it includes a target selection tool for prioritization of receptors for future drug discovery. This up-to-date knowledgebase will help identify strategies and trends in current GPCR drug discovery and give insights into which already drugged, or yet untapped targets have the largest potential in specific diseases.

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Caroli, J., Andreassen, S. N., Lorente, J. S., Xiao, B., Pandy-Szekeres, G., Gloriam, D.. 2025-01-14. An online GPCR drug discovery resource. https://doi.org/10.1101/2025.01.11.632537

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